摘要 |
<p>The claimed invention relates to the development of a novel substance, 4-((2-hydroxyethoxy)methyl)-5-methyl-2-methylmercapto-1,2,4-triazolo[1,5-a]pyrimidine-7(4H)-one, having the formula (I) and being intended for the treatment of West Nile Virus in humans and animals. A method for producing 4-((2-hydroxyethoxy)methyl)-5-methyl-2-methylmercapto-1,2,4-triazolo[1,5-a]pyrimidine-7(4H)-one consists in the deacetylation of 4-((2-acetoxyethoxy)methyl)-5-methyl-2-methylmercapto-1,2,4-triazolo[1,5-a]pyrimidine-7(4H)-one (II) under the action of a solution of an alkali metal methylate in aliphatic monovalent alcohol, wherein 4-((2-acetoxyethoxy)methyl)-5-methyl-2-methylmercapto-1,2,4-triazolo[1,5-a]pyrimidine-7(4H)-one (II) is produced by reacting 5-methyl-2-methylmercapto-1,2,4-triazolo[1,5-a]pyrimidine-7(4H)-one (III) with (2-acetoxyethoxy)methylacetate (IV) in the presence of a siliconizing agent, for example N,O-bis(trimethylsilyl)acetamide (BSA) or hexamethyldisilylamine (HMDS) and trimethylsilyl trifluoromethylsulfonate (TMSOTf) in an aprotic solvent. 4-((2-hydroxyethoxy)methyl)-5-methyl-2-methylmercapto-1,2,4-triazolo[1,5-a]pyrimidine-7(4H)-one can be used to treat West Nile Virus (WNV).</p> |
申请人 |
LIMITED LIABILITY COMPANY "URAL CENTER OF BIOPHARMACEUTICAL TECHNOLOGY" |
发明人 |
CHUPAKHIN, OLEG NIKOLAEVICH;RUSINOV, VLADIMIR LEONIDOVICH;ULOMSKY, EVGENY NARCISSOVICH;SAVATEEV, KONSTANTIN VALERIEVICH;BORISOV, STEPAN SERGEEVICH;NOVIKOVA, NATALIA ALEXANDROVNA;LOGINOVA, SVETLANA YAKOVLEVNA;BORISEVICH, SERGEY VLADIMIROVICH;SOROKIN, PAVEL VLADIMIROVICH |